Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10595557 | Bioorganic & Medicinal Chemistry Letters | 2013 | 7 Pages |
Abstract
Replacement of the dimethoxyphenyl moiety in the core skeleton of almorexant by appropriately substituted imidazoles afforded novel 1-chloro-5,6,7,8-tetrahydroimidazo[1,5-a]pyrazine derivatives as potent dual orexin receptor antagonists. We describe in this Letter our efforts to further optimize the potency and brain penetration of these derivatives by fine-tuning of the pivotal phenethyl motif, and we comment on the sleep-promoting activity of selected compounds in a rat electroencephalographic (EEG) model.
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Authors
Thierry Sifferlen, Ralf Koberstein, Emmanuelle Cottreel, Amandine Boller, Thomas Weller, John Gatfield, Catherine Brisbare-Roch, Francois Jenck, Christoph Boss,